(2S,3S)-2-(Diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (2S,3S)-2-(Diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine
• 英文别名: 2-benzhydryl-N-[(2-methoxyphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine
• 化学式: C₂₈H₃₂N₂O
• 分子量: 412.6
• InChiKey: FLNYLINBEZROPL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  24.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Substance P antagonists for the treatment of emesis
  申请人：PFIZER INC.

  公开号：EP0627221A2

  公开（公告）日：1994-12-07

  The present invention relates to compounds useful for treating or preventing emesis in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives and related compounds.

  本发明涉及利用某些喹吖啶衍生物、哌啶衍生物、氮杂环戊烷衍生物及相关化合物治疗或预防哺乳动物（包括人类）呕吐的化合物。
• NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis
  申请人：GLAXO GROUP LIMITED

  公开号：EP0916346A2

  公开（公告）日：1999-05-19

  The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists, processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(0)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

  本发明涉及速激肽拮抗剂（包括 P 物质拮抗剂和其他神经激肽拮抗剂）在治疗呃逆中的应用。本发明还描述了新型速激肽拮抗剂、其制备工艺、含有速激肽拮抗剂的药物组合物及其医疗用途。 其中 R 代表环 A 或 2-吡啶基或 2-吡啶基-N-氧化物； R1 选自卤素原子和 C1-4烷基、C1-4烷氧基、三氟甲基和 S(0)nC1-4 烷基； R2 和 R3（可以相同或不同）各自独立地选自氢和卤素原子以及 C1-4烷基、C1-4烷氧基、三氟甲基和氰基； n 代表 0、1 或 2； 及其药学上可接受的盐和溶剂。
• NK-1 receptor antagonist and a systemic antiinflammatory corticosteroid for the treatment of emesis
  申请人：GLAXO GROUP LIMITED

  公开号：EP0919245A2

  公开（公告）日：1999-06-02

  The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists, processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(0)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

  本发明涉及速激肽拮抗剂（包括 P 物质拮抗剂和其他神经激肽拮抗剂）在治疗呃逆中的应用。本发明还描述了新型速激肽拮抗剂、其制备工艺、含有速激肽拮抗剂的药物组合物及其医疗用途。 其中 R 代表环 A 或 2-吡啶基或 2-吡啶基-N-氧化物； R1 选自卤素原子和 C1-4烷基、C1-4烷氧基、三氟甲基和 S(0)nC1-4 烷基； R2 和 R3（可以相同或不同）各自独立地选自氢和卤素原子以及 C1-4烷基、C1-4烷氧基、三氟甲基和氰基； n 代表 0、1 或 2； 及其药学上可接受的盐和溶剂。
• NK1 Antagonists for the treatment of depression
  申请人：GLAXO GROUP LIMITED

  公开号：EP1082959A1

  公开（公告）日：2001-03-14

  The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of depression. Also described are novel tachykinin antagonists, processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(0)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1- 4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.

  本发明涉及速激肽拮抗剂（包括 P 物质拮抗剂和其他神经激肽拮抗剂）在治疗抑郁症中的应用。本发明还描述了新型速激肽拮抗剂、其制备工艺、含有速激肽拮抗剂的药物组合物及其医疗用途。 其中 R 代表环 A 或 2-吡啶基或 2-吡啶基-N-氧化物； R1 选自卤素原子和 C1-4烷基、C1-4烷氧基、三氟甲基和 S(0)nC1-4 烷基； R2 和 R3（可以相同或不同）各自独立地选自氢和卤素原子以及 C1-4 烷基、C1-4-烷氧基、三氟甲基和氰基； n 代表 0、1 或 2； 及其药学上可接受的盐和溶剂。
• Irrigation solution and use thereof for the perioperative inhibition of pain/inflammation and/or spasm at a vascular structure
  申请人：Omeros Corporation

  公开号：EP1609477A1

  公开（公告）日：2005-12-28

  A method and solution for perioperatively inhibiting a variety of pain and inflammation and spasm processes at a vascular structure during an intervascular procedure. The solution includes multiple pain and inflammation inhibitory agents and spasm inhibitory agents in a physiologic base, such as saline or lactated Ringer's solution. Depending on the application, the pain and inflammation agents included in the solution may include: (1) serotonin receptor antagonists; (2) serotonin receptor agonists; (3) histamine receptor antagonists; (4) bradykinin receptor antagonists: (5) kallikrein inhibitors; (6) tachykinin receptor antagonists, including neurokinin1 and neurokinin2 receptor subtype antagonists; (7) calcitonin gene-related peptide (CGRP) receptor antagonists; (8) interleukin receptor antagonists; (9) inhibitors of enzymes active in the synthetic pathway for arachadonic acid metabolites, including (a) phospholipase inhibitors, including PLA2 isoform and PLCγ isoform inhibitors, (b) cyclooxygenase inhibitors, and (c) lipooxygenase inhibitors; (10) prostanoid receptor antagonists including eicosanoid EP-1 and EP-2 receptor subtype antagonists and thromboxane receptor subtype antagonists; (11) leukotriene receptor antagonists including leukotriene B4 and D4 receptor subtype antagonists; (12) opioid receptor agonists, including mu-opiate, delta-opiate, and kappa-opiate receptor subtype agonists; (13) purinoceptor agonists and antagonists including P2X receptor antagonists and P2Y receptor agonists; (14) adenosine triphosphate (ATP) sensitive potassium channel openers; and (15) calcium channel antagonists. Suitable anti-inflammatory/anti-pain agents which also act as anti-spasm agents include serotonin receptor antagonists, tachykinin receptor antagonists, ATP-sensitive potassium channel openers and calcium channel antagonists. Other agents which may be utilized in the solution specifically for their anti-spasm properties including endothelin receptor antagonists and the nitric oxyde donors (enzyme activators). The solution is used to continuously irrigate a wound during an operative/interventional procedure for preemptive inhibition of pain and inflammation, as well as vascular and smooth muscle spasm, while avoiding undesirable side effects associated with oral, intramuscular or intravenous application of larger doses of the agents. The solution is useful for intravascular procedures.

  一种方法和溶液，用于在血管间手术期间围手术期抑制血管结构的各种疼痛、炎症和痉挛过程。该溶液包括生理基质（如生理盐水或乳酸林格氏液）中的多种疼痛和炎症抑制剂及痉挛抑制剂。根据不同的应用，溶液中包含的止痛和炎症抑制剂可包括(1) 血清素受体拮抗剂； (2) 血清素受体激动剂； (3) 组胺受体拮抗剂； (4) 缓激肽受体拮抗剂：(5) 降凝血酶抑制剂；(6) 速激肽受体拮抗剂，包括神经激肽 1 和神经激肽 2 受体亚型拮抗剂；(7) 降钙素基因相关肽（CGRP）受体拮抗剂；(8) 白细胞介素受体拮抗剂；(9) 花生四烯酸代谢物合成途径中活性酶的抑制剂，包括：(a) 磷脂酶抑制剂，包括 PLA2 同工酶和 PLCγ 同工酶抑制剂；(b) 环氧化酶抑制剂；(c) 脂氧化酶抑制剂；(10) 类固醇受体拮抗剂，包括类二十烷酸 EP-1 和 EP-2 受体亚型拮抗剂和血栓素受体亚型拮抗剂； (11) 白三烯受体拮抗剂，包括白三烯 B4 和 D4 受体亚型拮抗剂；(12) 阿片受体激动剂，包括μ-阿片、δ-阿片和卡帕-阿片受体亚型激动剂； (13) 嘌呤受体激动剂和拮抗剂，包括 P2X 受体拮抗剂和 P2Y 受体激动剂； (14) 对三磷酸腺苷（ATP）敏感的钾通道开放剂；以及 (15) 钙通道拮抗剂。合适的消炎/止痛剂也可作为抗痉挛剂，包括血清素受体拮抗剂、速激肽受体拮抗剂、ATP 敏感性钾通道开放剂和钙通道拮抗剂。溶液中可使用的其他抗痉挛药剂包括内皮素受体拮抗剂和一氧化氮供体（酶激活剂）。该溶液用于在手术/介入治疗过程中持续冲洗伤口，以预先抑制疼痛和炎症以及血管和平滑肌痉挛，同时避免口服、肌肉注射或静脉注射大剂量药剂所带来的不良副作用。该溶液适用于血管内手术。